Abstract

Objective: This study aimed to evaluate the cytotoxic activity of peniocerol against human colon cancer cell lines and its antitumor effect in vivo in a xenograft model using nu/nu mice.Materials and Methods: SW-620, HCT-15, and HCT-116 colon cancer cell lines were treated with peniocerol for cytotoxicity by crystal violet technique. Cell apoptosis induction was detected by flow cytometry, and the antitumor activity of peniocerol was evaluated in a xenograft model of HCT-116 in nu/nu mice. After treatment, the effect of peniocerol was analyzed in histological sections of tumors by immunohistochemistry using DAPI, anti-PCNA, and PARP-1 antibodies.Results: Peniocerol inhibited cell growth and induced apoptosis in vitro in a time and dose-dependent manner. Besides, peniocerol administration (30 or 15 mg/kg) inhibited tumor growth and induced apoptosis in the xenograft mice. The lack of peniocerol toxicity was proved by a biochemical blood analysis of healthy nu/nu mice administrated with this sterol.Conclusions: Our results proved that peniocerol induces apoptosis in vitro and in vivo assays.

Highlights

  • Colorectal cancer (CC) is second cancer with the highest mortality rate worldwide, responsible for more than 880 thousand deaths, and is the third most common cancer, with almost 2 million incidents in both sexes and all ages [1]

  • HCT116 cells treated with peniocerol experimented apoptosis in a time-dependent manner

  • The level of apoptosis induced by peniocerol was similar to that produced by camptothecin (Figure 2B)

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Summary

Introduction

Colorectal cancer (CC) is second cancer with the highest mortality rate worldwide, responsible for more than 880 thousand deaths, and is the third most common cancer, with almost 2 million incidents in both sexes and all ages [1]. Several chemotherapeutic options are available, 5-fluorouracil (5-FU) is still the base drug for the treatment of colorectal cancer in combination with other anticancer agents. The combination of oxaliplatin, 5-FU, and leucovorin is used after tumor surgery for patients undergoing treatment with curative intent for stage III [2]. The drug with the desirable activity and adequate toxicity has not been developed yet. Searching for better antitumor drugs is not concluded.

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